Home Ubiquitin DUB inhibitor ML364 For research use only.

ML364

ML364 is a small molecule inhibitor of the deubiquitinase USP2 with an IC50 of 1.1 μM in a biochemical assay using an internally quenched fluorescent di-ubiquitin substrate.

ML364 Chemical Structure

ML364 Chemical Structure

CAS No. 1991986-30-1

Purity & Quality Control

ML364 Related Products

Signaling Pathway

DUB Signaling Pathways

DUB Signaling Pathway

Biological Activity

Description ML364 is a small molecule inhibitor of the deubiquitinase USP2 with an IC50 of 1.1 μM in a biochemical assay using an internally quenched fluorescent di-ubiquitin substrate.
Targets
USP8 [1]
(Cell-free assay)		 USP2 [1]
(Cell-free assay)
0.95 μM 1.1 μM
In vitro
In vitro

ML364 induces an increase in cellular cyclin D1 degradation and causes cell cycle arrest in Mino and HCT116 cancer cell lines. ML364 is antiproliferative in cancer cell lines. ML364 also causes a decrease in homologous recombination-mediated DNA repair. It is inactive against caspase 6, caspase 7, MMP1, MMP9, and USP15, but does inhibit USP8 with an IC50 of 0.95 μM. In a panel of 102 kinases that included regulators of the cell cycle there is no binding observed to any of the enzymes tested using 10 μM ML364[1].
Cell Research Cell lines LnCAP cells and MCF7 cells
Concentrations 0-20 μM
Incubation Time 24 h
Method

ML364 promotes degradation of cyclin D1 in LnCAP cells and MCF7 cells. Cells are treated with ML364 for 24 h, and cyclin D1 protein levels are assessed by Western blotting using a tubulin control.

Chemical Information & Solubility

Molecular Weight 517.54 Formula

C24H18F3N3O3S2
CAS No. 1991986-30-1 SDF --
Smiles CC1=CC=C(C=C1)S(=O)(=O)NC2=C(C=CC(=C2)C(F)(F)F)C(=O)NC3=NC(=CS3)C4=CC=CC=C4
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 60 mg/mL ( (115.93 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 15 mg/mL

Water : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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